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Opioids Flashcards

1
Q

What is nociception ?

A

Non- conscious neural traffic due to trauma due to trauma or potential trauma to tissue

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2
Q

What is pain?

A

complex unpleasant awareness of sensation modified by variable experiences , context, etc.

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3
Q

how is pain generated ?

A

Via Spinothalmic tract:

  1. Nociceptors stimulated
  2. Release of sub P and glutamate
  3. afferent nerves stimulated
  4. fibres decussate
  5. AP ascends and synapse in thalamus
  6. project to Post central gyrus
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4
Q

what modulates pain peripherally ?

A

Substantia gelantinosa- dorsal horn

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5
Q

what modulates pain centrally ?

A

peri adueductal grey

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6
Q

what do A(delta) and c fibres ?

A

send stimulatory signals up from nociceptors the spinothalmic tract
inhibit the Substantia gelantinosa

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7
Q

how does rubbing your knee help reduce pain ?

A

stimulate AlphaBeta fibres which stimulates substantia geletanosa to modulate the pain from A(delta) and C nerves to reduce signals of pain

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8
Q

how do when modulate pain centrally ?

A

Cortex usually inhibits peri aqueductal Grey matter . During pain , thalamus and cortex send stimulatory signals to PAGM which inhibits spinal cord to reduce pain signals via 5-HT and endogenous opioids

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9
Q

Name the endogenous opioids

A

Enkephalins
Dynorphins
B endorphins

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10
Q

what are the 3 Opioid receptors ?

A 
Mop = mu
DOP= delta
KOP= kappa
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11
Q

outline how opioid receptors work

A

Hyperpolarisation and decrease of substance P

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12
Q

what does Mop receptors modulate ?

A

analgesia , depression , euphoria , dependence , respiratory sedation

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13
Q

Whta do Dop receptors modulate ?

A

analgesia, inhibit dopamine, modulate Mop

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14
Q

what do Kop receptors modulate ?

A

analgesia , duiresis , dysphoria

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15
Q

what is the order of WHO analgesic ladder ?

A

Simple analgesia
weak opioid = codeine
strong Opioid

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16
Q

what should you use for neuropathic pain e.g diabetic neuropathy ?

A

Anticonvulsants
tricyclics
SSRIs, NARI

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17
Q

what other indications can you use opioids ? what receptor is the main one affected ?

A

cough , diarrhoea and palliation

Mop

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18
Q

what is the absorption of morphine ? bioavailibilty ?

A

PO, IV, IM , SC, PR
Gut absorption erratic-
40%

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19
Q

what is the distribution of morphine ?

elimination ?

A

rapidly enters all tissues including foetal
struggles to enter BBB
Renally

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20
Q

what is the metabolism of morphine ?

what molecules

A

significant first pass effect

combines with glucuronic acid –> M6G (Analesgic) and M3G (Neuro stimulatory and irritabilty )

21
Q

what is the MOA of morphine and what is its actions ?

A

Strong affinity to Mop and less so Dop and Kop

Analgesia and Euphoria

22
Q

what are Respiratory side effects of morphine and how do they occur ?

A

resp depression

medullar resp centre less responsive to CO2

23
Q

what are GI side effects of morphine and how do they occur ?

A

Emesis - stimulate chemoreceptor trigger zone decrease motility and increase sphincter tone = constipation , nausea

24
Q

what other side effects are seen in morphine ?

A

Miosis

Histamine- be careful in asthmatics

25
what is the Absorption of fentanyl ?
IV, Epidural, Intrathecal , Nasal | 80-100% bioavail
26
What is the distribution if fentanyl like ?
highly lipophilic , highly protein bound and CNS crossing high
27
What is the metabolism and Elimination like in fentanyl ?
Met = CYP3A4 | Renally excreted
28
What are features of fentanyl compared to morphine ?
100x more potent high affinity for Mop less histamine , sedation and constipation
29
what are side effects of Fentanyl ?
resp depression Constipation vomiting
30
what enzyme metabolises Codeine ? what inhibits said enzyme ?
CYP2D6 | Fluoxetine , SSRIs
31
how is codeine eliminated ?
glucoronidation and renal exertion
32
what is codeine metabolised to ?
Codein to morphine via CYP2D6
33
what are the actions of codiene?
Cough depressant | Mild/mod analgesia
34
what are side effects of morphine ?
Constipation | resp depression - esp in children , dont give under 12
35
what is the pharmokinetics of Buprenorphine ? ADME
A- Transdermal D- Very lipophilic M- Via CYP3A4 E- Biliary system so safe in renal impairment
36
what are features of Buprenorphine compared to morphine ?
Very high affinity to Mop = low Kd, not displaced long action duration low Emax as it is partial agonist Antagonist at Kop
37
what are indications for buprenorphine ?
Moderate to sever pain polypharmacy patients Opioid addiction
38
what are side effects of Buprenorphine ?
Resp depression Low Bp Nausea dizziness
39
what is the absorption of Naloxone ?
IV, IM , IN, PO Low oral bioavail (First pass) rapid onset of action
40
What is the D, M and E of Naloxone ?
D= rapid due to lipophilicity | M and E= renally excreted, within 30-60 Mins
41
what are features of Naxolone ?
affinity MOP>DOP>KOP | Greater affinity than morphine , less than Buprenorphine
42
What must you be aware of naxolone in acute setting ?
short acting so give long infused dose to avoid secondary OD
43
How does opioid tolerance build ?
Up regulation of opioid receptors when using opioids leads to more Mop receptors = increased mount of opioid for cellular response
44
how can stopping an opioid lead to withdrawls ?
endogenous opioids cannot initiate a cellular response
45
what is given to opioid addicts during withdrawl and how does it work ?
Methadone is given to stop withdrawal effects leading without much of a high . weaning of slowly to allow Mop receptors to down-regulate
46
what patients should you be considerate of when prescribing opioids ?
``` Manual labourers/Drivers • Elderly • Bedbound • Asthmatics • Biliary tract obstruction • Respiratory Diseases • Renal impairment • Pregnancy ```
47
what are contraindications of opioids?
Hepatic failure acute respiratory distress comatose Head injuries , raised ICP = M3G causes irritability
48
what should you in do palliative prescribing for opioids ?
ignore special considerations laxatives if in pain and SOB

Nervous system (20 decks)

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